Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid
Patent
1990-08-27
1993-03-23
Michl, Paul R.
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Organic pressurized fluid
424 70, 424468, 424470, 514317, 514355, 514356, A61L 904
Patent
active
051961849
DESCRIPTION:
BRIEF SUMMARY
The invention refers to a pharmaceutical preparation containing Nifedipin as the active substance together with a solution promoter, such as, for example, copolyvidon or polyvinylpyrrolidone and/or glycerol-polyethyleneglycoloxystearate, and with a solvent, such as, for example, alcohols, in particular ethanol, or polyalcohols, as well as, optionally, propelling agent for spraying in form of individually doseable sprays for sublingual application.
Medicines containing Nifedipin are known in quite different compositions and for varying types of application. A preparation of the initially mentioned type can, for example, be derived from WO 87/05211. In this preparation according to the known prior art there was introduced an improvement such that Nifedipin being present in a sprayable condition, i.e. being mixed with a propelling agent, remains in solution and will, after the spraying jet, not easily be again precipitated. It is known that Nifedipin is poorly soluble in water and it is further known that a preparation containing Nifedipin as a solution gives rise to precipitating reactions of the Nifedipin with the saliva. In this connection, there was stated in "Deutsche Apothekerzeitung" 128.sup.th annual, No. 23, on page 38, that the various known oral dosage forms are occasionally described even in packing enclosures as being sublingually active and that this activity could not be confirmed. Non-sustained released Nifedipin capsules for sublingual application proposed for the acute therapy of the hypertensive crisis and of angina pectoris ought, according to such packing enclosures, result in a more rapid resorption after having broken the capsule with the teeth and having kept the content of the capsule within the mouth for some time, which effect could not be proved in practice. This is attributed to the circumstance that the known preparations are subject to precipitating reactions and that the desired resorption is prevented by a relatively rapid growth of the crystals of the Nifedipin.
For the purpose of accelerating the resorption of pharmaceuticals there has, in particular with respect to dermatological applications, already become known a number of auxiliary substances and there has in particular been proposed benzyl alcohol as a resorption accelerator. A resorption-accelerating activity has, for example, been described in EP-A 183 527 in connection with calcitonin. The preparation having become known from this EP-A 183 527 is a preparation which is resorbed via the mucous membrane of the nose.
From DE-OS 2 209 526, there have become known coronary agents, which are said to be rapidly perlingually resorbable, i.e. via the tongue and via the mucous membrane of the throat. Control tests have now shown that the agents having become known from DE-OS 2 209 526 are, on the one hand, not suitable for the production of a spray even when using propelling agents and result, on the other hand, together with the saliva of the oral cavity in a rapid cristal growth of the Nifedipin and in a precipitation.
The conditions to be considered for the composition of a preparation, which simultaneously shall be suitable to be mixed with a propelling agent, shall mantain the Nifedipin in solution and shall reliably prevent precipitation reactions on dilution with water or the saliva of the mouth, respectively, are partially contradictory, and more recently serious doubts have been expressed with respect to a greater afflux velocity of known preparations containing Nifedipin in case of sublingual application. Such a doubt can, for example, also be taken from "Deutsche Apothekerzeitung" 128.sup.th annual, No. 24, page 1268, where can be found the distinct statement that sublingual applications of the known preparations result in lower plasma levels as compared to an oral application. A further problem existing with preparations being intended for being sprayed in doses by means of a pump without using a propelling gas results from the fact that the viscosity and the surface tension of the preparation can, for the purpose
REFERENCES:
patent: 4264611 (1981-04-01), Berntsson
patent: 4272516 (1981-06-01), Caldini
patent: 4755544 (1988-07-01), Makino
patent: 4832954 (1989-05-01), Sato
patent: 4869899 (1989-09-01), Burghart
patent: 4871545 (1989-10-01), Dethlefsen
patent: 4877799 (1989-10-01), Drejer
Burghart Kurt
Burghart Walter
Benston William E.
Michl Paul R.
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